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Home / Biochemicals / Small Molecules

GABA(A)-Compound 1b

SKU : BHB21300109

A Novel Antagonist of GABA(A) Receptors

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Mfr.No.	CMG-004, CMG-004_10 mg, CMG-004_25 mg, CMG-004_5 mg, CMG-004_50 mg
Description	GABA(A)-Compound 1b (#CMG-004) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C20H12F3N3O2S.
Pubchem Cid	136118605
Synonyms	Synthetic
Background	GABA(A)-Compound 1b (8-methyl-5-(4-(trifluoromethyl)-1-benzothiophen-2-yl)-1,9-dihydro-2H-(1,3)oxazolo(4,5-h)(2,3)benzodiazepin-2-one) is a potent and selective antagonist of alpha5 containing GABA(A) receptors, displaying an IC50 value of 201 nM. On alpha1-4 containing receptors, the antagonist demonstrates only partial maximum inhibition1.GABA(A)-Compound 1b is characterized as a 2,3-benzodiazepine with substantial blood-brain barrier permeability. In vivo studies reveal that 1b is devoid of sedative effects, is pro-convulsive, and enhances the performance of rats in the object recognition test.GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter throughout the central nervous system (CNS), thus play an important role in inhibiting cell excitation in the CNS.GABA(A) receptors are considered a major target of antiseizure drugs2.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	0.1-10 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
Molecular Weight	415.39
Solubility	Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
Target	GABA(A) receptors
Activity	A novel antagonist of alpha5 containing GABA(A) receptors, displaying significant selectivity for alpha5 (IC50 = 201 nM, Imax = 92%) over alpha1, alpha2, alpha3 and alpha4 containing receptors, on which it produces only partial maximum inhibition (Imax = 54, 0, 39 and 35%, respectively) at higher concentrations (IC50 = 0.48, >10, 0.48 and 0.91 uM, respectively)1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: 8-Methyl-5-(4-(trifluoromethyl)-1-benzothiophen-2-yl)-1,9-dihydro-2H-(1,3)oxazolo(4,5-h)(2,3)benzodiazepin-2-one.

Purity	>98% (HPLC)
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Ling, I. et al. (2015) Eur. J. Pharmacol. 764, 497. Williams, M. et al. (1989) J. Pharmacol. Exp. Ther. 248, 89. Ling, I. et al. (2015) Eur. J. Pharmacol. 764, 497.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300109-1	CMG-004_10 mg	10 mg	$509		Add to Cart
BHB21300109-2	CMG-004_25 mg	25 mg	$1019		Add to Cart
BHB21300109-3	CMG-004_5 mg	5 mg	$287		Add to Cart
BHB21300109-4	CMG-004_50 mg	50 mg	$1648		Add to Cart

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